1. Field of the Invention
The present invention relates to piperidinium compounds and in particular their use in compositions for topical application, in particular antiperspirants. Preferred piperidinium compounds include 1,1-dimethyl-4-[2-cyclopentyl-2-hydroxyphenylacetyl)oxy]-piperidinium salts and 1,1-dimethyl-4-[3-methyl-2-phenylvaleryl)oxy]-piperidinium salts, in particular 1,1-dimethyl-4-[(2-cyclopentyl-2-hydroxyphenylacetyl)oxy]-piperidinium bromide. Their use in therapeutically active or cosmetic compositions is advantageous.
2. Discussion of Background Information
Various chemical compounds for treating bladder diseases are known from U.S. Pat. No. 6,482,837, the entire disclosure whereof is incorporated by reference herein. Substituted N-methyl-4-piperidinium compounds, inter alia, are disclosed therein, a plurality of molecular residues and combinations and variations of these residues being described. The compounds disclosed in U.S. Pat. No. 6,482,837 serve all medical purposes and in particular the treatment of bladder diseases.
Furthermore, from the literature are known 4-[cyclopentylhydroxyphenylacetyl)oxy]-1,1-dimethyl-piperidinium with CAS number 807285-21-8 and 4-hydroxy-1,1-dimethylpiperidinium iodide, α-cyclopentyl mandelate with CAS number 113569-69-0 and 1,1-dimethyl-4-[3-methyl-2-phenylvaleryl)oxy]-piperidinium bromide with CAS number 100337-30-2. However, further information regarding these compounds, in particular on their possible applications, are not found in the literature.
In humans two different sweat glands are responsible for the development of perspiration and perspiration odor, which are more or less pronounced, depending on the area of the body. The eccrine sweat glands secrete mainly salt and water and usually do not contribute to the formation of odor. The apocrine sweat glands are responsible for the odor, which secrete fatty acids, cholesterines and other compounds. These substances are decomposed by bacteria on the skin, the breakdown products producing the odor typical of perspiration.
In order to suppress perspiration odor over a longer period, the use of cosmetic preparations is essential. The conventional cosmetic deodorants are based on different mechanisms of action that can also be combined: on the one hand deodorizing agents are used that suppress the growth of the bacteria causing the perspiration odor. These antimicrobial (bacteriostatic) agents include, e.g., triclosan, chlorhexidine and naturally occurring compounds such as farnesol and phenoxyethanol.
On the other hand, antiperspirants are used which prevent the secretion of sweat by blocking the sweat gland ducts. In the large majority of antiperspirants, the formation of perspiration is reduced by the use of so-called astringents—primarily aluminum salts such as aluminum hydroxychloride (aluminum chlorohydrate) or aluminum/zirconium salts.
Also the combination of astringents with antimicrobially active substances in one and the same composition is customary. Furthermore, fragrances are used to mask the perspiration odor.
However, the aluminum chlorohydrate conventionally used as an antiperspirant has various disadvantages due to the acid character and the active mechanism, which range from the known yellowish textile staining to perfume instabilities to a limited selection of formulas. It is a particular drawback for the user that residues can stain clothing in an unpleasant way and the low pH value (very acidic) of the cosmetic preparation negatively impacts the biological balance of the skin.
It would be desirable to provide compounds that are toxicologically harmless, can be easily incorporated without complications into therapeutically active or cosmetic preparations, are easy to synthesize and moreover have one or more additional advantageous properties. It would be particularly advantageous to provide substances for use in therapeutic or cosmetic compositions that have the effect of reducing or inhibiting perspiration.
It would also be desirable to provide effective cosmetics and in particular antiperspirant products that do not exhibit the disadvantages of the prior art and preferably render superfluous the necessity of the use of antiperspirant agents based on aluminum compounds or at least help to reduce them.